Tachykinin receptor 3, also known as TACR3, is a
protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, respo ...
which in humans is encoded by the ''TACR3''
gene
In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth'' or ''gender'') can have several different meanings. The Mendelian gene is a ba ...
.
Function
This gene belongs to a family of genes that function as
receptor
Receptor may refer to:
* Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse
*Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a ...
s for
tachykinin
Tachykinin peptides are one of the largest families of neuropeptides, found from amphibians to mammals. They were so named due to their ability to rapidly induce contraction of gut tissue. The tachykinin family is characterized by a common C-termi ...
s. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neurokinin 3, also referred to as
neurokinin B
Neurokinin B (NKB) belongs in the family of tachykinin peptides. Neurokinin B is implicated in a variety of human functions and pathways such as the secretion of gonadotropin-releasing hormone.
Additionally, NKB is associated with pregnancy in fem ...
.
Selective ligands
A number of selective ligands are available for NK
3. NK
3 receptor antagonists are being investigated as treatments for various indications.
Agonists
*
Neurokinin B
Neurokinin B (NKB) belongs in the family of tachykinin peptides. Neurokinin B is implicated in a variety of human functions and pathways such as the secretion of gonadotropin-releasing hormone.
Additionally, NKB is associated with pregnancy in fem ...
– endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK
3
*
Senktide – 7-amino acid polypeptide, NK
3 selective, CAS# 106128-89-6
Antagonists
*
Elinzanetant (BAY-3427080 GSK-1144814, NT-814)
*
Fezolinetant (ESN-364)
*
Osanetant
Osanetant (developmental code name SR-142,801) is a Tachykinin receptor 3, neurokinin 3 receptor receptor antagonist, antagonist which was developed by Sanofi-Synthélabo and was being researched for the treatment of schizophrenia but was discont ...
(SR-142,801)
*
Pavinetant
Pavinetant (, ; developmental code names MLE-4901, AZD-4901, AZ-12472520, AZD-2624), is a small-molecule, oral administration, orally active, binding selectivity, selective tachykinin receptor 3, neurokinin-3 (NK3) tachykinin receptor 3, receptor ...
(MLE-4901, AZD-4901, AZD-2624)
*
Talnetant
Talnetant (SB-223,412) is a neurokinin 3 receptor antagonist developed by GlaxoSmithKline, which is being researched for several functions (primarily treatment of irritable bowel syndrome, despite a 2007 study finding no statistically significan ...
(SB-223,412)
*
SB-222,200 – potent and selective antagonist, K
i = 4.4 nM, 3-Methyl-2-phenyl-N-
1S)-1-phenylpropyl4-quinolinecarboxamide, CAS# 174635-69-9
*
SB-218,795 – more selective than SB-222,200, K
i = 13 nM, (R)-
2-Phenyl-4-quinolinylcarbonyl)aminomethyl ester benzeneacetic acid, CAS# 174635-53-1
See also
*
Tachykinin receptor
There are three known mammalian tachykinin receptors termed NK1, NK2 and NK3. All are members of the 7 transmembrane G-protein coupled receptor family and induce the activation of phospholipase C, producing inositol triphosphate (so called Gq- ...
References
Further reading
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External links
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G protein-coupled receptors
{{transmembranereceptor-stub